♦Amifostine
(a-mee-phos’-tin)
Ethyol
Pregnancy Category C
Mechanism of Action
Amifostine is dephosphorylated at the tissue site by alkaline phosphatase to form free thiol. Once inside the cell, the free thiol binds with and neutralizes the reactive species of cis-platin. It also acts as a potent scavenger of oxygen free radicals. This action is important because free radicals can damage cell membranes, DNA, and other important cell components, which will lead to cell death.
Indications
Used to reduce the cumulative renal toxicity associated with cisplatin-based therapies in advanced ovarian cancer or non-small cell lung cancer. It is also indicated to alleviate moderate xerostomia associated with radiation therapy.
Metabolism/Excretion
Rapidly cleared from the plasma. Elimination half-life: about 88 minutes. Excreted by the renal system.
Dosage Range
♦ With cisplatin therapy: 910 mg/m2 given as a 15-minute infusion once a day 30 minutes before the cisplatin-based treatment.
♦ For moderate xerostomia: 200 mg/m2 given as a 3-minute IV infusion starting 15 to 30 minutes before standard fraction radiation therapy.
♦ Use in children, elderly patients, and patients with pre-existing cardiovascular or cerebrovascular conditions has not been evaluated.
Drug Preparation/Stability